The coordination chemistry of the diatopic heteroscorpionate ligand 4-(N,N-bis-(2-pyridyl)-amino)methylbenzoic acid (HL) with CdX2 (X = Cl、Br、I)has been investigated for the construction of higher order metallosupramolecular architectures. Six new compounds were obtained by hydrothermal reacti...

Four coordination complexes, namely, [Cu(HBCB)]n (1), {[Cu(HBCB)(o-bimb)]·H2O} (2), {[Cu1.5(BCB)(m-bimb)1.5]·DMF}n (3), and [Co1.5(BCB)(bpy)1.5(H2O)]n (4), have been assembled from the semirigid tripodal 3,5-bis(2-carboxylphenoxy)benzoic acid (H3BCB) in the presence or absence of the N-donors ...

The new ligands 3-(3-(2-pyridyl)pyrazol-1-ylmethyl)benzoic acid (L2) and 5-(3-(2-pyridyl)pyrazol-1-ylmethyl)benzene 1,3-dicarboxylic acid (L3) are reported and the synthesis and characterisation of [PdCl2(L)] and [PtCl2(L)] complexes of these and the previously reported 4-(3-(2-pyridyl)pyrazol-1...

Histaminergic (HA) neurons located in the tuberomamillary nucleus (TMN) of the posterior hypothalamus fire exclusively during waking and support many physiological functions. We investigated the role of the endovanilloid N-oleoyldopamine (OLDA) in TMN, where dopamine synthesis and its conjugatio...

A small library of novel hybrid spiroheterocycles containing spirooxindole, pyrrolidine and indole/imidazole moieties were synthesized with complete regio- and diastereoselectively in good to excellent yields from a three-component process starting from a series of variously substituted (E)-(2-n...

Peptaibols are an intriguing class of fungal metabolites due both to their wide range of reported bioactivities and to the structural variability that can be generated by the exchange of variable amino acid building blocks. In an effort to streamline the discovery of structurally diverse peptaib...

Temperature- and pH-sensitive homopolymer having chiroptical property was synthesized by reversible addition–fragmentation chain transfer (RAFT) polymerization of a threonine-containing acrylamide, N-acryloyl-l-threonine (A-(L)Thr-OH), followed by methylation. The LCST-type thermoresponsive pro...

Overexpression of leucine-zipper and sterile-α motif kinase (ZAK) in heart has been closely associated with the development of hypertrophic cardiomyopathy (HCM). N-(3-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl) benzene-sulfonamides, novel highly selective ZAK inhibitors, had exhibited reasonable o...

Stable NH-form of the threonine-based Schiff base 4, (2S,3R)-3-((tert-butyldimethylsilyl)oxy)-2-(((E)-(2-hydroxynaphthalen-1-yl)methylene)amino)butanamide, was synthesized and characterized in the crystalline state by means of IR spectroscopy and X-ray crystallographic analysis. This is the firs...

Three threonine aldolases (TAs) were cloned and overexpressed in Escherichia coli (Aeromonas jandaei l-allo-threonine aldolase, E. coli l-threonine aldolase and Thermotoga maritima l-allo-threonine aldolase). A Design of Experiments strategy was used to identify optimal reaction conditions for e...

We designed chiral 2-nitroimidazole derivatives containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety as antiangiogenic hypoxic cell radiosensitizers. Based on results of molecular orbital calculations, the 2-aminomethylene-4-cyclopentene-1,3-dione moiety is expected to show high electro...

In an effort to understand the oxidation chemistry of new generation biofuels, oxidation of a pentanol isomer (2-methyl-1-butanol) was investigated experimentally in a jet-stirred reactor (JSR) at a pressure of 10 atm, equivalence ratios of 0.5, 1, 2 and 4 and in a temperature range of 700–1200...

Photooxidation of cyclopentadiene has been carried out in methanol using white light of LED lamp, rose bengal as photo initiator, and compressed air at 0 °C. Under conditions of [thiourea] ≫ [cyclopentadiene], the consumption of thiourea follows a pseudo-first-order reaction kinetics with half ...

The bacteriostatic and fungistatic activities of a number of β-naphthol, 2-hydroxy-6-naphthoic acid, and 2-hydroxy-3-naphthoic acid derivatives are reported against Staphylococcus aureus, Salmonella typhosa, and Aspergillus niger. Selected compounds from the initial screening have been further ...

The bacteriostatic and fungistatic activities of a number of β-naphthol and 2-hydroxy-3-naphthoic acid derivatives are reported against Bacillus typhosus, Micrococcus pyogenes, var. aureus, and Aspergillus niger. Selected compounds from the initial screening were further tested for their activi...

7-Bromomethylbenz[a]anthracene was less carcinogenic than the parent hydrocarbon, 7-methylbenz[a]anthracene, whereas 7-bromomethyl-12-methylbenz[a]anthracene was a potent carcinogen, giving 100% incidence of sarcoma in the rat after a single subcutaneous injection. The chemical reactivities of t...

Colloidal dispersions of polycyclic aromatic hydrocarbons were found to inhibit glyceraldehyde-3-phosphate dehydrogenase (GPDH) and lactic acid dehydrogenase (LDH) after a short exposure of the incubation medium to laboratory lighting. The activation effect was observed with substituted 7-methyl...

In order to study the influence of fluorine substitution at the meso-position of benz[a]anthracene and at the 12-position of 7-methylbenz[a]anthracene on the carcinogenic properties of these hydrocarbons, the title compounds have been prepared by photocyclization of 1-(1-f1uoro-2-naphthyl)-2-(o-...

[3+2] reactions play a key role in constructing various pharmaceutical moleculars. In this study, using Mn(OAc)3 mediated and 1,3-dipolar [3+2] cyclization reactions, 38 novel dihydrofuran and dihydroisoxazole analogues of isoCA-4 were synthesized as inhibitors of tubulin polymerization. Among t...

The tributylphosphane-promoted [3 + 2] annulation reactions of 3-hydroxyoxindoles with acrylates have been developed to give a variety of pharmaceutically attractive spirocyclic oxindole-lactone derivatives in good to excellent yields. The structures of all the compounds were confirmed by 1H NMR...